38652-79-8

Usage

Uses

Used in Neuroscience Research:
1-(2-DIETHYLAMINO-ETHYL)-1H-BENZOIMIDAZOL-2-YLAMINE is used as a research ligand for targeting the serotonin 5-HT7 receptor, which is crucial for modulating mood, cognition, and sleep. Its agonistic properties allow researchers to study the receptor's role in these physiological processes and explore potential therapeutic applications for related disorders.
Used in Drug Development:
1-(2-DIETHYLAMINO-ETHYL)-1H-BENZOIMIDAZOL-2-YLAMINE is used as a potential antagonist for the adenosine A1 receptor in drug development. Its antagonistic activity is significant for understanding the receptor's involvement in heart rate regulation and immune response, which can lead to the creation of medications that address conditions related to these physiological functions.
Used in Pharmaceutical Industry:
1-(2-DIETHYLAMINO-ETHYL)-1H-BENZOIMIDAZOL-2-YLAMINE is used as a lead compound in the development of new medications targeting the central nervous system. Its dual functionality as both a serotonin 5-HT7 receptor agonist and an adenosine A1 receptor antagonist positions it as a valuable asset in the search for treatments for mood disorders, cognitive impairments, sleep disorders, and conditions related to heart rate and immune system regulation.

InChI:InChI=1/C13H20N4/c1-3-16(4-2)9-10-17-12-8-6-5-7-11(12)15-13(17)14/h5-8H,3-4,9-10H2,1-2H3,(H2,14,15)

Upstream product

• 162976-69-4 1H-benzimidazol-2-ylcarbamic acid methyl ester 
• 934-32-7 1H-benzimidazol-2-amine 
• 100-35-6 2-(diethylamino)ethyl chloride 
• 1069-72-3 2-bromo-N,N-diethylethan-1-amine hydrochloride 
• 869-24-9 2-chloro-N,N-diethylethylamine hydrochloride 
• 40828-54-4 1H-benzimidazole-2-sulfonic acid 

Relevant academic research and scientific papers

Synthesis, DNA binding and in vitro antiproliferative activity of purinoquinazoline, pyridopyrimidopurine and pyridopyrimidobenzimidazole derivatives as potential antitumor agents

In the search for new antitumor agents, 8,10-dimethylpurino[7,8- a]quinazoline-5,9,11(6H,8H,10H)-triones 1, 8,10-dimethyl- pyrido[2',3':4,5]pyrimido[1,2-f]purine-5,9,11(6H,8H,10H)-triones 2, and 5,7- dihydro-5-oxopyrido[3',2':5,6]pyrimido[1,2-a]benzimidazoles 3, a series of new planar heteropolycyclic compounds, were synthesized. The approach to understanding their structure-activity relationship involved a physico- chemical investigation of the binding process of these molecules to DNA, considered to be an important target for drug action, and an examination of their biological activity. Thermodynamic parameters of the DNA binding process, intrinsic binding constant and exclusion parameter were determined. The mode of interaction was additionally investigated by means of linear flow dichroism studies. Evaluation of the biological activity included cell growth inhibition in human tumoral cell lines and the ability to indUCe DNA cleavage in the presence of eukaryotic topoisomerase II. Only compounds of the purinoquinazoline series 1, which are able to form a complex with DNA and to inhibit the topoisomerase II, show antiproliferative activity.

The derivatives of imidazo[1,2-a]benzimidazole as 5-HT2A receptor antagonists

We studied in vitro the 5-HT2A antagonistic activity of 16 imidazo[1,2-a]benzimidazole derivatives. Using the radioligand method we showed the binding of 9-(2-diethylaminoethyl)-2-(4-methoxyphenyl)imidazo[1,2-a]benzimidazol dinitrate to the 2A subtype serotonin receptor.

Synthesis and pharmacological activity of 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazoles

An efficient method for the synthesis of novel 9H-imidazo[1,2-a]benzimidazole derivatives containing a biphenyl substituent at position 2 was developed. These compounds, belonging to the privileged substructures, have been tested for a wide range of pharmacological activities in the in vitro test panel. It was shown that the synthesized derivatives demonstrated high antioxidant activity, some of them inhibit type 1B protein tyrosine phosphatase, activate AMP-activated protein kinase, possess antiplatelet properties, and a rare and very interesting kind of activity, the ability to break cross-links of glycated proteins. The most active compounds can be suggested for further optimization.

NOVEL ANTI-INFECTIVE COMPOUNDS AND METHODS USING SAME

The present invention includes a method of treating or preventing a bacterial infection in a subject in need thereof. The method comprises administering to the subject a therapeutically effective amount of at least one compound of the invention. In certain embodiments, the bacterium is Gram-negative. In other embodiments, the bacterium is obligatory aerobic.

Synthesis, in vitro antiplatelet activity and molecular modelling studies of 10-substituted 2-(1-piperazinyl)pyrimido[1,2-a]benzimidazol-4(10H)-ones

The multistep preparation of the new 10-substituted 2-(1-piperazinyl) pyrimido[1,2-a]benzimidazol-4(10H)-ones 6a-o, and of the two isomers 10-ethyl-2-(diethylamino)pyrimido[1,2-a]benzimidazol-4(10H)-one 6p and 10-ethyl-4-(diethylamino)pyrimido[1,2-a]benzimidazol-2(10H)-one 13, as well as the in vitro evaluation of their inhibitory activity on human platelet aggregation induced in platelet-rich plasma by ADP, collagen or the Ca 2+ ionophore A23187 were here described. Nine out of fifteen 2-(1-piperazinyl)derivatives (6g-o) showed good inhibitory properties towards all the platelet aggregation agonists used. Moreover, a molecular modelling study has been performed on two of the best compounds of this series (6i and 6o) to confirm in silico their interactions with the catalytic site of human platelet PDE3, using the X-ray data of the PDE3B isoform in complex with an inhibitor.

Synthesis and some conversions of N-substituted benzimidazole-2-sulfonic acids

A series of N-substituted benzimidazole-2-sulfonic acids was synthesized in good yield by the N-alkylation of benzimidazole-2-sulfonic acids by alkylation with simple and functionalized alkylating agents under mild conditions. The corresponding N-substitu

Benzimidazole compounds

Compounds of the general formula (I): STR1 wherein A, B, C, D, n, R1, R2, R3, R4, X, Y and Z are as defined in the description, and their use as antidiabetics are disclosed.